Editorial: FourthWinter Conferenceon Medicinal and Bioorganic

Chemistry. Part 1

This issue and the following issue of Medicinal Research Reviews are dedicated to plenary lectures

that were presented at the Fourth Winter Conference on Medicinal and Bioorganic Chemistry, held

January 28±February 2, 2001, in Steamboat Springs, Colorado. Symposia from the conference

included Target-Driven Approaches to Anticancer Agents, Pharmacokinetics for Medicinal

Chemists, Recent Advances in the Structural Biology of Seven Transmembrane Receptors, and

Nuclear Hormone Receptors. Professor Dale Boger (Scripps Research Institute) delivered the

keynote address at this conference, highlighting synthetic and mechanistic aspects in his research on

vancomycin, teicoplanin, and ramoplanin.

This issue presents the keynote address by Professor Dale Boger and seminal papers from the

symposia on Pharmacokinetics for Medicinal Chemists and Recent Advances in the Structural

Biology of Seven Transmembrane Receptors. The pharmacokinetics papers are provided by Dr.

David Lau and Dr. Gondi Kumar and their co-workers at Amgen, Inc. The paper by Lau provides an

excellent primer for medicinal chemists who need to understand the noncompartmental and

compartmental pharmacokinetic models of compound disposition and incorporate this science into

their practice of drug discovery. The paper by Kumar provides a similar primer on the molecular

basis of drug metabolism, including analysis of pharmacophore models for drug metabolism by

major cyp P450 enzymes and strategies for optimizing the metabolic disposition of small molecules.

Dr. Thomas Thompson (Quintiles, Inc.) also provides an invited paper on the topic of metabolic

stability of small molecules, and describes the evolution of this science in modern drug discovery.

Reports from the symposium on Recent Advances in the Structural Biology of Seven

Transmembrane Receptors include a paper by Professor Dale Mierke (Brown University), detailing

structural characterization of peptide hormone binding to G-protein coupled receptors by NMR

techniques, and also a paper by Dr. Oren Becker (Bio Information Technologies), which describes a

suite of computational tools for generating de novo 3D structures of G-protein coupled receptors

from receptor primary sequence.

The following issue of Medicinal Research Reviews will present papers from the symposia

Target-Driven Approaches to Anticancer Agents and Nuclear Hormone Receptors.

The Steamboat Springs Winter Conference Series on Medicinal and Bioorganic Chemistry is

sponsored by the Medicinal Chemistry Foundation. The Foundation and Medicinal Research

Reviews trust that you will ®nd the papers in this issue of value to your research endeavors.

Daniel Flynn, Guest Editor

Millennium Pharmaceuticals, INC

355

Medicinal Research Reviews, Vol. 21, No. 5, 355, 2001ß 2001 John Wiley & Sons, Inc.